1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. VEGFR

VEGFR

Vascular endothelial growth factor receptor

VEGFRs consist of three subtypes, the fms-like tyrosine kinase Flt-1 (VEGFR1/Flt-1), the kinase domain region, also referred to as fetal liver kinase (VEGFR2/KDR/Flk-1), and Flt-4 (VEGFR3). Each receptor has seven immunoglobulinlike domains in the extracellular domain, a single transmembrane region, and a consensus tyrosine kinase sequence interrupted by a kinase insert domain. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. The VEGF family members VEGF-A, -B, -C, -D, -E, and PlGF, and the human immunodeficiency (HIV) Tat protein bind in specific patterns to three related receptor protein tyrosine kinases, VEGFR1, 2, and 3, and induce the formation of homo- and heteromeric receptor complexes. Binding of VEGF to VEGFR causes dimerization and autophosphorylation of the receptor. Intracellular proteins such as VEGFR-associated protein (VRAP), PLC, and Sck that associate with specific tyrosine residues of VEGFR are phosphorylated upon receptor activation. Several signal transduction pathways are activated by the binding of VEGF to its receptor, leading to increased proliferation, survival, permeability, and migration of cells.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-142085
    Antiproliferative agent-20
    Inhibitor
    Antiproliferative agent-20 is a potent and orally active anticancer agent. Antiproliferative agent-20 exhibits antiproliferative and anti-angiogenic activities.
    Antiproliferative agent-20
  • HY-P992086
    Anti-Mouse VEGF Antibody (G6-31)
    Inhibitor
    Anti-Mouse VEGF Antibody (G6-31) is a anti-mouse VEGF antibody. Anti-Mouse VEGF Antibody (G6-31) blocks VEGF-A-mediated angiogenesis and shows antitumor activity. Anti-Mouse VEGF Antibody (G6-31) can be used for the research of cancer, such as multiple endocrine neoplasia type 1.
    Anti-Mouse VEGF Antibody (G6-31)
  • HY-P10052
    CBO-P11
    Inhibitor
    CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. CBO-P11 is modified with a nearinfrared cyanine dye bearing an alkyne function, allowing both “click” coupling on azido-modified nanoparticles and fluorescence labelling.
    CBO-P11
  • HY-N2575R
    Hypocrellin A (Standard)
    Inhibitor
    Hypocrellin A (Standard) is the analytical standard of Hypocrellin A. This product is intended for research and analytical applications. Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml)[1][2][3][4][5][6][7][8][9].
    Hypocrellin A (Standard)
  • HY-146228
    HSP90-IN-13
    Inhibitor
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway.
    HSP90-IN-13
  • HY-P990543
    Anti-VEGFR2/KDR/CD309 Antibody (AT001)
    Inhibitor
    The Anti-VEGFR2/KDR/CD309 Antibody (AT001) is a humanized antibody expressed in CHO cells that targets VEGFR2/KDR/CD309. The Anti-VEGFR2/KDR/CD309 Antibody (AT001) contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-VEGFR2/KDR/CD309 Antibody (AT001) can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-VEGFR2/KDR/CD309 Antibody (AT001)
  • HY-W706452
    Cabozantinib-d4 S-malate
    Cabozantinib-d4 (S-malate) (XL184-d4 (S-malate); BMS-907351-d4 (S-malate)) is the deuterium labeled Cabozantinib (S-malate) (HY-12044). Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
    Cabozantinib-d<sub>4</sub> S-malate
  • HY-117733
    Zerumin A
    Inhibitor
    Zerumin A is an anti-angiogenic agent that acts on multiple molecular targets related to angiogenesis (including kdr/VEGFR2, angpt1, angpt2, tie1, and tie2). Zerumin A specifically inhibits the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by regulating the VEGF-VEGFR and ANGPT-TIE signaling pathways, and dose-dependently inhibits angiogenesis (10-20 μM significantly inhibits zebrafish embryo angiogenesis). Zerumin A can be used in the research of cancer and angiogenesis-related inflammatory diseases. Zerumin A can be naturally extracted from the 95% ethanol extract of the fruits, seeds, and pericarp of Alpinia caerulea (R.Br.) Bentham (a plant of the Alpinia genus in the Zingiberaceae family).
    Zerumin A
  • HY-155684
    SA-PA
    Inhibitor
    SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues.
    SA-PA
  • HY-P992485
    XENP9493
    XENP9493 is an IgG antibody against hVEGFA.
    XENP9493
  • HY-145849
    VEGFR2-IN-1
    Inhibitor
    VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition.
    VEGFR2-IN-1
  • HY-183369
    VEGFR/PD-L1-IN-1
    Inhibitor
    VEGFR/PD-L1-IN-1 is a VEGFR2 and PD-L1 inhibitor, with IC50 values of 0.383 μM and 134.407 pg/mL against VEGFR2 and PD-L1, respectively. VEGFR/PD-L1-IN-1 enhances the secretion of INF-γ, induces G0/G1 cell cycle arrest in cancer cells, and triggers cancer cell apoptosis. VEGFR/PD-L1-IN-1 upregulates the expression of BAX and Caspase-3, and downregulates the expression of Bcl-2. VEGFR/PD-L1-IN-1 can be used in research related to hepatocellular carcinoma, prostate cancer, and colorectal cancer.
    VEGFR/PD-L1-IN-1
  • HY-178004
    VEGFR-2-IN-73
    Inhibitor
    VEGFR-2-IN-73 is a potent and selective VEGFR-2 inhibitor, showing selectively inhibition of VEGFR-2 (IC50 = 0.0787 μM) over EGFR (IC50 = 1.31 μM). VEGFR-2-IN-73 demonstrates potent antiproliferative activity across multiple cancer cell lines. VEGFR-2-IN-73 induces G2/M and Pre-G1 phase arrest and significantly enhances apoptosis. VEGFR-2-IN-73 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer.
    VEGFR-2-IN-73
  • HY-178142
    Multi-kinase-IN-7
    Inhibitor
    Multi-kinase-IN-7 is a multikinase inhibitor with IC50s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC50 values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.
    Multi-kinase-IN-7
  • HY-170662
    VEGFR-2-IN-62
    Inhibitor
    VEGFR-2-IN-62 (Compound 3f) is an effective VEGFR-2 inhibitor with an IC50 value of 0.0557 μM. VEGFR-2-IN-62 can inhibit cell proliferation and induce apoptosis, and can be used in cancer research.
    VEGFR-2-IN-62
  • HY-16265A
    JI-101 hydrochloride
    Inhibitor
    JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity.JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis.JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes.JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route.JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors.
    JI-101 hydrochloride
  • HY-179140
    EGFR/VEGFR2-IN-8
    Inhibitor
    EGFR/VEGFR2-IN-8 (compound 10k) is a dual EGFR/VEGFR-2 inhibitor (EGFR IC50 = 57 nM, VEGFR-2 IC50 = 21 nM). EGFR/VEGFR2-IN-8 has anti proliferative activity against various tumor cells, such as MCF-7 (IC50 = 20 nM), Panc-1 (IC50 = 22 nM), A-549 (IC50 = 23 nM), HT-29 (IC50 = 23 nM) cells. EGFR/VEGFR2-IN-8 has antioxidant and apoptosis inducing activity. EGFR/VEGFR2-IN-8 can be used for research on various types of cancer.
    EGFR/VEGFR2-IN-8
  • HY-162326
    VEGFR-2-IN-41
    Inhibitor
    VEGFR-2 IN-41 (Compound 8) is a VEGFR-2 inhibitor with an IC50 of 0.0554 μM. VEGFR-2 IN-41 can induce apoptosis. VEGFR-2-IN-41 has antitumor activity.
    VEGFR-2-IN-41
  • HY-P990088
    Sotiburafusp alfa
    Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa also functions as a PD-L1 inhibitor and a VEGF inhibitor.
    Sotiburafusp alfa
  • HY-165413
    KST012174 hydrochloride
    Inhibitor
    KST012174 hydrochloride is a potent HIF-1α-p300/CBP interaction inhibitor with an IC50 of 107 μM. KST012174 hydrochloride completely blocks the binding of HIF-1α to p300 protein at a concentration of 100 μM, without affecting the expression stability of HIF-1α protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of HIF-1α and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies.
    KST012174 hydrochloride
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